2G12-2B2-L0H3-MMAE

2G12-2B2-L0H3-MMAE is a humanized antibody-drug conjugate (ADC) composed of the anti-Sialyl-Tn (STn) antibody 2G12-2B2-L0H3 linked to the cytotoxic payload monomethyl auristatin E (MMAE) via a cleavable linker. The antibody targets the Sialyl-Tn glycan antigen, which is overexpressed on certain cancer cells, including ovarian carcinoma. Upon binding to STn-positive tumor cells, the ADC is internalized, and MMAE is released inside the cell, where it inhibits microtubule polymerization, inducing apoptosis. The drug is designed to selectively deliver a potent anti-mitotic agent to tumor cells, limiting off-target toxicity. Preclinical studies have shown marked anti-tumor efficacy in cell line- and patient-derived ovarian cancer xenograft models. The drug is administered intravenously and demonstrates a terminal half-life of approximately 2.5 days in mouse PK studies. Preclinical safety studies in monkeys indicate a favorable toxicity profile at specific dosing levels, with the primary adverse effects being hematologic at higher exposures.